Atosiban
Atosiban: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Atosiban
ATX code: G02CX01
Active ingredient: Atosiban (Atosiban)
Manufacturer: CJSC Obninsk Chemical-Pharmaceutical Company (Russia); LLC "Pharmidea" (Latvia)
Description and photo update: 2020-28-05
Atosiban is a drug that suppresses labor. It is a blocker of oxytocin receptors.
Release form and composition
The drug is produced in the form of a concentrate for the preparation of a solution for infusion, which is a colorless, transparent solution (0.9 ml each in transparent colorless glass vials with a capacity of 2 ml, sealed with a bromobutyl stopper and hermetically sealed with a flip-off lid; 5 ml each in transparent colorless glass bottles with a capacity of 6 ml, sealed with a bromobutyl stopper and hermetically sealed with a flip-off lid; in a cardboard box 1 bottle and instructions for use of Atosiban; for hospitals: in cardboard boxes 9, 21 or 121 bottles of 0, 9 ml or 4, 10 or 64 vials of 5 ml).
Composition for 1 ml of concentrate:
- active substance: atosiban (in the form of atosiban acetate) - 7.5 mg;
- auxiliary components: 1M hydrochloric acid solution (until pH 4.5 is reached), mannitol, water for injection.
Pharmacological properties
Pharmacodynamics
Atosiban is a synthetic peptide. It is a competitive antagonist of human oxytocin. The drug acts at the receptor level. Atosiban binds to oxytocin receptors, reducing the tone of the myometrium and the frequency of uterine contractions, which ultimately leads to suppression of uterine contractility. In addition, it binds to vasopressin receptors, inhibiting the action of vasopressin, but does not affect the cardiovascular system.
With the development of premature birth as a result of the use of the drug in the recommended doses, the contraction of the uterus is suppressed and its functional rest is ensured. Immediately after the administration of atosiban, the uterus begins to relax. The contractile activity of the myometrium is significantly reduced during the first 10 minutes, and then a stable functional dormancy of the uterus is maintained for 12 hours (4 or less contractions per hour).
Pharmacokinetics
Pharmacokinetics of the drug (clearance, half-life and volume of distribution) does not depend on the dose.
After intravenous (intravenous) infusion at a dose of 300 mcg / min for 6-12 hours, the maximum plasma concentration is reached within the first hour after the start of the infusion. The range of maximum plasma concentration ranges from 298 to 533 ng / ml (the average is 442 ± 73 ng / ml). Atosiban passes through the placenta to the fetus, while the ratio of the concentration of the active substance in the fetus to the concentration of the drug in the mother's body is 0.12. About 46–48% of Atosiban binds to plasma proteins. The average value of the volume of distribution is 18.3 ± 6.8 liters.
2 metabolites are found in urine and blood. The pharmacological activity of one of the metabolites is comparable to that of atosiban itself.
The concentration of the drug in the blood plasma rapidly decreases after the termination of the intravenous infusion. The initial half-life is 0.21 ± 0.01 hours, the final one is 1.7 ± 0.3 hours. The average clearance is 41.8 ± 8.2 l / h. In urine, unchanged Atosiban is found in very small amounts (its concentration is 50 times lower than the concentration of the active metabolite).
Indications for use
Atosiban is used in case of a threat of premature birth in pregnant women over the age of 18 years for a period of 24-33 full weeks, subject to normal heart rate (heart rate) in the fetus in the following situations:
- uterine contractions are regular, the duration of the contractions is at least 30 seconds, and the frequency is more than 4 times within 30 minutes;
- cervical dilatation no more than 1-3 cm (for nulliparous women - no more than 0-3 cm).
Contraindications
Absolute:
- premature placental abruption;
- placenta previa;
- uterine bleeding, which requires immediate delivery;
- suspicion of inflammation of the chorioamniotic membranes;
- eclampsia or severe preeclampsia requiring urgent delivery;
- abnormal heart rate in the fetus;
- intrauterine growth retardation;
- intrauterine fetal death;
- premature rupture of membranes during pregnancy more than 30 weeks;
- pregnancy less than 24 weeks or more than 33 weeks (full);
- any condition of the fetus or mother, in which the continued preservation of pregnancy is dangerous to the life and health of the fetus or mother;
- lactation period;
- a history of indication of hypersensitivity to the main or auxiliary components of the drug.
Relative (Atosiban is used with caution):
- impaired renal or liver function;
- multiple pregnancy;
- suspicion of premature rupture of the membranes (the need to prolong pregnancy should be compared with the potential risk of inflammation of the chorioamniotic membranes);
- gestational age 24–27 weeks (as there is insufficient clinical experience);
- joint use with other tocolytic drugs.
Atosiban, instructions for use: method and dosage
The drug is administered intravenously, in three stages.
The introduction of atosiban is started immediately after the diagnosis of preterm labor is confirmed:
- 1st stage: 0.9 ml of undiluted concentrate (1 bottle) is injected within 1 min, i.e. the initial dose is 6.75 mg;
- 2nd stage: a 3-hour infusion is performed at a dose of 300 μg / min (the dose of atosiban is 18 mg / h, the rate of administration is 24 ml / h);
- 3rd stage: a continuous intravenous infusion (up to 45 hours) is carried out at a dose of 100 μg / min (the dose of atosiban is 6 mg / h, the rate of administration is 8 ml / h).
The total duration of all three stages should be no more than 48 hours. The maximum course dose of atosiban is 330.75 mg.
If it is necessary to re-use the drug, treatment is started again from the 1st stage, and then the 2nd and 3rd stages are carried out.
Re-introduction of atosiban can be started at any time after the end of the first course. It is recommended to carry out no more than 3 cycles of therapy. If after the 3rd cycle the contractile activity of the uterus does not decrease, it is necessary to consider the possibility of using another tocolytic agent.
To prepare the infusion solution, you can use 5% glucose solution, Ringer's acetate solution, or 0.9% sodium chloride solution. To do this, 10 ml are drained from a bottle with 100 ml of solvent, and then 2 bottles (10 ml) of Atosiban are injected to obtain an infusion solution with a concentration of 75 mg / 100 ml. The prepared solution can be stored for no more than 24 hours. If the color changes or any particles appear, the infusion solution should be disposed of.
Side effects
- digestive system: very often - nausea; often - vomiting;
- metabolism and nutrition: often - increased blood sugar;
- cardiovascular system: often - lowering blood pressure, tachycardia, hot flashes;
- nervous system: often - dizziness, headache; infrequently - insomnia;
- genitals and mammary gland: very rarely - uterine atony / uterine bleeding;
- skin and subcutaneous fat: infrequently - itching, rash;
- immune system: rarely - allergic reactions;
- others: often - an increase in temperature at the injection site; infrequently - fever.
Overdose
Several cases of atosiban overdose have been recorded, but there are no specific signs of intoxication.
In case of drug intoxication, supportive and symptomatic treatment is performed. The antidote is unknown.
special instructions
If during the administration of the solution the contractile activity of the uterus does not decrease, it is necessary to monitor the contractions of the uterus and control the heart rate in the fetus. If necessary, the possibility of using other drugs of tocolytic action is considered.
In the case of intrauterine growth retardation of the fetus, in order to make a decision to resume or continue therapy, it is necessary to assess the degree of maturity of the fetus.
Atosiban should not be used in patients with abnormal attachment of the placenta.
Since atosiban is an oxytocin antagonist, it can promote uterine relaxation and provoke postpartum uterine bleeding. In women in labor who were injected with the drug, after delivery, the degree of blood loss should be regularly assessed.
Influence on the ability to drive vehicles and complex mechanisms
Given the indications of Atosiban, driving and performing other potentially dangerous and complex work during the period of drug use is impossible.
Application during pregnancy and lactation
Atosiban is contraindicated until 24 full weeks and after 33 full weeks of pregnancy. In the interval from 24 to 33 weeks, the drug is used only if the diagnosis of "premature birth" is confirmed.
Breastfeeding is an absolute contraindication to the use of atosiban.
Pediatric use
It is not recommended to prescribe the drug to pregnant women under the age of 18, as there is no data on the safety and effectiveness of Atosiban in such patients.
With impaired renal function
In patients with impaired renal function, the use of Atosiban requires caution.
For violations of liver function
Atosiban is administered with caution to pregnant women with impaired liver function.
Drug interactions
The drug Atosiban does not affect the pharmacokinetic parameters of drugs, in the metabolism of which cytochrome P450 is involved.
Interaction of Atosiban with antibiotics is unlikely.
When combined with labetalol, the pharmacokinetics of the drug does not change. There were no clinically significant drug interactions with betamethasone.
The drug is inappropriate to use simultaneously with ergot alkaloids, since the indications and pharmacological properties of these drugs are opposite.
Analogs
The analogue of Atosiban is Tractocil.
Terms and conditions of storage
Store in a dark place, out of the reach of children, at a temperature of + 2 … + 8 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Atosiban
Reviews about Atosiban are mainly left by doctors, who note its high efficiency in the treatment of threatening premature birth. In one of the studies conducted, in about 90% of the observed patients, the drug helped to prolong pregnancy, while there were no side effects. It is noted that in order to achieve the desired effect, it is important to follow the Atosiban administration scheme (not a single step should be skipped).
The main disadvantage is the high cost of the drug, but taking into account the costs of nursing deeply premature babies, it fully justifies itself.
The price of Atosiban in pharmacies
The price of Atosiban in the form of a concentrate for the preparation of a solution for infusion 7.5 mg / ml in 0.9 ml vials (1 vial in a package) is 910-1000 rubles, in 5 ml vials (1 vial in a package) - 5600 –5800 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
